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32

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6196	PP1 EI 275,AGL 1872	Apoptosis; EGFR; Bcr-Abl; Src; c-Kit	Angiogenesis; Apoptosis; Cytoskeletal Signaling; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	PP1 (AGL 1872) 是一种选择性有效 Src 家族抑制剂，抑制 Lck 和Fyn，IC50分别为 5 和 6 nM。
T2153	1-NM-PP1 PP1 Analog II,1 nM-PP1	Serine/threonin kinase; CDK; Src	Angiogenesis; Cell Cycle/Checkpoint; Metabolism; Tyrosine Kinase/Adaptors
	1-NM-PP1 (PP1 Analog II) 是一种有效的Src 家族激酶抑制剂，是一种细胞渗透性 PP1 类似物，对 v-Src-as1 与 c-Fyn-as1 的IC50值分别为 4.3 nM、3.2 nM。
T3935	1-Naphthyl PP1 4 -氨基- 1 -叔丁基- 3 -(1' -萘基)吡唑并[3,4 - D]嘧啶,1-NA-PP 1	Src	Angiogenesis; Tyrosine Kinase/Adaptors
	1-Naphthyl PP1 (1-NA-PP 1) 是选择性的src 家族激酶抑制剂，能够抑制 v-Src (IC50:1.0 μM)、c-Fyn (IC50:0.6 μM)、c-Abl (IC50:0.6 μM)、CDK2 (IC50:18 μM) 和 CAMK II (IC50:22 μM)。
T7371	1-Naphthyl PP1 hydrochloride 1-叔丁基-3-(1-萘基)-1H-吡唑并[3,4-D]嘧啶-4-胺盐酸盐,1-NA-PP 1 hydrochloride	Src	Angiogenesis; Tyrosine Kinase/Adaptors
	1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) 是选择性的 src 家族激酶抑制剂，能够抑制 v-Src (IC50:1.0 μM)、c-Fyn (IC50:0.6 μM)、c-Abl (IC50:0.6 μM)、CDK2 (IC50:18 μM)、CAMK II (IC50:22 μM)。
T21678	3MB-PP1	PLK	Cell Cycle/Checkpoint
	3MB-PP1是嘌呤类似物，是一种 Polo 样激酶 1 (Plk1) 抑制剂。在表达类似物敏感的 Plk1 等位基因的细胞中，3MB-PP1 通过靶向 Plk1 阻断有丝分裂进程和细胞分裂。3MB-PP1 特异性抑制类似物敏感的 Ssn3 (Cdk8)。3MB-PP1 抑制 Leu93 突变 Zipper-interacting protein kinase(Leu93-ZIPK)，IC50为2 μM。3MB-PP1 可用于细胞分裂和白色念珠菌 (Candida albicans) 菌丝形成的研究。
T41113	3BrB-PP1 3BrB-PP1
	3BrB-PP1 is an ATP-competitive analog that exhibits specific inhibitory activity towards protein kinase. It is effective in inhibiting protein kinase with mutations in the ATP-binding pocket, specifically the mutation of Thr97 within Sty1's ATP-binding pocket.
T60718	3-IN-PP1
	3-IN-PP1是一种针对蛋白激酶D（PKD）家族成员PKD1、PKD2和PKD3具有高效抑制作用的抑制剂，IC50值分别为108、94和108 nM。此外，3-IN-PP1作为一种广谱抗癌剂，能抑制多种肿瘤细胞的生长，适用于癌症研究领域。
T14022	2OH-BNPP1	Others	Others
	2OH-BNPP1 是BUB1 kinase 抑制剂，可用于研究癌症。
T2415	PP121	Apoptosis; VEGFR; Bcr-Abl; PDGFR; Src; mTOR; Hck	Angiogenesis; Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	PP121是一种多靶点激酶抑制剂，抑制 PDGFR、Hck、mTOR、VEGFR2、Src、Abl、DNK-PK 的 IC50值分别为2、8、10、12、14、18、60 nM。
T28818	SMAPP1
	SMAPP1 is an activator of protein phosphatase 1 (PP1). SMAPP1 induces PP1 activity in vitro and activates latent HIV-1 provirus in cultured and primary T cells.
TP1963	[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide cpp1-7-npy19-23-ala31-aib32-gln34-hpancreatic-polypeptide,[cPP1-7,NPY19-23,Ala31,Aib32,Gln34] - hPancreatic Polypeptide
	Potent, selective peptide agonist for the neuropeptide Y Y5 receptor (IC50 values for inhibition of NPY binding to human Y5, Y1, Y2 and Y4 receptors are 0.24, 530, > 500, and 51 nM respectively, Ki at Y5 = 0.1 - 0.15 nM). Stimulates food intake in vivo.
T61782	NPP1-IN-1
	NPP1-IN-1 is a highly potent inhibitor of NPP enzymes, effectively inhibiting NPP1 with an IC 50 value of 0.15 μM and NPP3 with an IC 50 value of 40 μM [1].
T80291	PP113
	PP113是一种具有广谱抗菌性的抗菌肽，能有效作用于多种革兰氏阴性及革兰氏阳性细菌。对E.coli (MIC: 73.3 uM)、B. subtilis (MIC: 23.3 uM)、S. aureus (MIC: 13 uM)、S. lutea (MIC: 16.7 uM)及B. pumilus (MIC: 23.3 uM)表现出不同程度的最小抑菌浓度(MIC)。
T69560	ENPP1 inhibitor 43
	ENPP1 inhibitor 43 is a novel small molecule for cancer immunotherapy.
T37431	ENPP1 Inhibitor C ENPP1 Inhibitor C
	ENPP1 inhibitor C is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; IC50 = 0.26 μM in a cell-free assay).1 It is selective for ENPP1 over ENPP2-7 at 10 μM. ENPP1 inhibitor C decreases ENPP1 activity in MDA-MB-231 human breast and C6 rat glioma cancer cells when used at a concentration of 10 μM. \|1. Kawaguchi, M., Han, X., Hisada, T., et al. Development of an ENPP1 fluorescence probe for inhibitor screening, cellular imaging, and prognostic assessment of malignant brea...
T75913	[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic polypeptide TFA
	[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide 为高效且选择性的神经肽 YY5 受体激动剂，其与 hY5 受体的结合 IC50 值为 0.24 nM，已知可促进饮食摄入。
T80288	PP13
	PP13是一种具有广谱抗菌活性的抗菌肽，有效针对多种革兰氏阴性及革兰氏阳性细菌，包括E.coli (MIC: 16.7 uM)、B. subtilis (MIC: 13.3 uM)、S. aureus (MIC: 23.3 uM)、S. lutea (MIC: 8.0 uM)以及B. pumilu (MIC: 9.0 uM)。
T80290	PP102
	PP102为一种抗菌肽，针对革兰氏阴性及革兰氏阳性细菌展现出抗菌效能，具体作用于B. subtilis（MIC: 25 uM）、S. aureus（MIC: 13 uM）、S. lutea（MIC: 63 uM）和B. pumilu（MIC: 23 uM）。
T3045	Salubrinal	Apoptosis; Phosphatase; PERK; Autophagy; HSV	Apoptosis; Autophagy; Metabolism; Microbiology/Virology
	Salubrinal 是一种磷酸酶抑制剂，对真核翻译起始因子 2 亚基 (eIF2α) 发挥作用。它作为双特异性磷酸酶 2 抑制剂，抑制抗胶原蛋白抗体诱导的关节炎。它具有抗HSV-1病毒的活性，并抑制由HSV-1蛋白 ICP34.5 介导的eIF2α的去磷酸化。
T32108	HXJ42 HXJ-42,HXJ 42	Others	Others
	HXJ42 是一种 PP1 类似物，可选择性地有效作用于野生型 ZAP-70 (AS)。
T2747	Endothall	Others	Others
	Endothall 是一种有效的蛋白磷酸酶 2A (PP2A) 抑制剂，对 PP2A 和 PP1 具有抑制作用， IC50 分别为 90 nM 和 5 µM。Endothall 具有抗癌活性，可用于癌症化疗，可用作除草剂。
T14859	Calyculin A (-)-Calyculin A	Others	Others
	Calyculin A is a potent and cell-permeable inhibitor of protein phosphatase 1 (PP1; IC50s: 2 nM). It also is a protein phosphatase 2A (PP2A) inhibitor (IC50s: 0.5-1 nM).
T13095	Tautomycin	Others	Others
	Tautomycin is a potent and specific protein phosphatases 1 and 2A inhibitor (Kiapp of 0.16 nM and 0.4 nM for PP1 and PP2A, respectively), and is an antifungal antibiotic isolated from the bacterium Streptomyces verticillatus.
T70441	1E7-03
	1E7-03 is an inhibitor of HIV-1 transcription, by targeting host Protein Phosphatase-1 (PP1).
T68749	EBOV-IN-C31
	EBOV-IN-C31 is a novel PP1-targeting Ebola Virus (EBOV) inhibitor with improved pharmacological properties.
TP2054	Calcineurin Autoinhibitory Peptide
	Selective inhibitor of Ca2+-calmodulin-dependent protein phosphatase (calcineurin) (IC50 ~ 10 μM). Does not inhibit PP1, PP2A or CaM kinase II (IC50 > 100 mM).
TP1698	Microcystin-LA
	Microcystin LA, a natural toxin, exerts its cytotoxic exects by inhibiting the serine-threonine protein phosphatases PP1 and PP2A with IC50s of 0.3 and 0.3 nM, respectively.
T68458	Fostriecin (free base)
	Fostriecin (free base) is an inhibitor of the serine/threonine protein phosphatases 2A (PP2A) and 4 (PP4) (IC50s = 3.2 and 3 nM, respectively). It less effectively inhibits topoisomerase II and PP1 (IC50s = 40 and 131 μM, respectively) and does not inhibit PP2B. Through its effects on protein phosphatases, fostriecin increases the level of histone H3 phosphorylation and may alter epigenetic regulation of cell proliferation. On a related note, fostriecin was first identified as an antitumor antib...
T68721	Cantharidin imide
	Cantharidin imide is a PP1/2A inhibitor found in Canarthis vesicatoria. It inhibits proliferation of colorectal cancer cells, increases MCP-1, IL-6, and IL-β levels, and inhibits differentiation and resorptive activity of osteoclasts. This compound can produce severe skin inflammation, and is extremely toxic if ingested orally.
T39183	Okadaic acid ammonium salt
	Okadaic acid ammonium salt, a marine toxin, serves as an inhibitor of protein phosphatases (PP), displaying a higher affinity for PP2A (IC 50 =0.1-0.3 nM) alongside inhibitory effects on PP1 (IC 50 =15-50 nM), PP3 (IC 50 =3.7-4 nM), PP4 (IC 50 =0.1 nM), and PP5 (IC 50 =3.5 nM), but does not affect PP2C. By inhibiting PPs, this compound promotes protein phosphorylation and acts as a tumor promoter. Additionally, it is involved in inducing tau phosphorylation.
T35777	Nodularin
	The cyanobacterium Nodularia spumigena often contaminates the drinking water of rural communities in developing countries and accumulates in mussels, flounder, and cod from the northern Baltic Sea. Nodularin is a hepatotoxic monocylic pentapeptide produced by the N. spumigena. It is a potent inhibitor of protein phosphatase types 1 (PP1) and 2A (PP2A), exhibiting IC50 values of 1.8 and 0.026 nM, respectively. PP2B is inhibited to a lesser extent with an IC50 of 1.8 μM. No apparent inhibitory eff...
T35613	Cytostatin (sodium salt)
	Cytostatin is a natural antitumor inhibitor of cell adhesion to extracellular matrix, blocking adhesion of B16 melanoma cells to laminin and collagen type IV in vitro (IC50s = 1.3 and 1.4 μg/ml, respectively) and B16 cells metastatic activity in mice. It induces apoptosis of FS3 mouse fibrosarcoma cells (IC50 = 3.1 μg/ml). Cytostatin potently and selectively inhibits protein phosphatase 2A (PP2A; IC50 = 29 nM against the catalytic subunit), while having no effect against PP1, PP2B, or PP5.

化合物

Cat.No: T6196

Synonym: EI 275,AGL 1872

Target: Apoptosis, EGFR, Bcr-Abl, Src, c-Kit

Cat.No: T2153

Synonym: PP1 Analog II,1 nM-PP1

Target: Serine/threonin kinase, CDK, Src

Cat.No: T3935

Synonym: 4 -氨基- 1 -叔丁基- 3 -(1' -萘基)吡唑并[3,4 - D]嘧啶,1-NA-PP 1

Target: Src

1-Naphthyl PP1 hydrochloride

Cat.No: T7371

Synonym: 1-叔丁基-3-(1-萘基)-1H-吡唑并[3,4-D]嘧啶-4-胺盐酸盐,1-NA-PP 1 hydrochloride

Target: Src

Cat.No: T21678

Target: PLK

Cat.No: T41113

Synonym: 3BrB-PP1

Cat.No: T60718

Cat.No: T14022

Target: Others

Cat.No: T2415

Target: Apoptosis, VEGFR, Bcr-Abl, PDGFR, Src, mTOR, Hck

Cat.No: T28818

[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide

Cat.No: TP1963

Synonym: cpp1-7-npy19-23-ala31-aib32-gln34-hpancreatic-polypeptide,[cPP1-7,NPY19-23,Ala31,Aib32,Gln34] - hPancreatic Polypeptide

Cat.No: T61782

Cat.No: T80291

ENPP1 inhibitor 43

Cat.No: T69560

ENPP1 Inhibitor C

Cat.No: T37431

Synonym: ENPP1 Inhibitor C

[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic polypeptide TFA

Cat.No: T75913

Cat.No: T80288

Cat.No: T80290

Cat.No: T3045

Target: Apoptosis, Phosphatase, PERK, Autophagy, HSV

Cat.No: T32108

Synonym: HXJ-42,HXJ 42

Target: Others

Cat.No: T2747

Target: Others

Cat.No: T14859

Synonym: (-)-Calyculin A

Target: Others

Cat.No: T13095

Target: Others

Cat.No: T70441

Cat.No: T68749

Calcineurin Autoinhibitory Peptide

Cat.No: TP2054

Cat.No: TP1698

Fostriecin (free base)

Cat.No: T68458

Cantharidin imide

Cat.No: T68721

Okadaic acid ammonium salt

Cat.No: T39183

Cat.No: T35777

Cytostatin (sodium salt)

Cat.No: T35613

Cat. No.	Product Name	Target	Signaling Pathways
T4839	Ac-Ala-OH N-Acetylalanine,N-Acetyl-L-alanine,N-乙酰-L-丙氨酸	Others; Endogenous Metabolite	Metabolism; Others
	Ac-Ala-OH (N-Acetyl-L-alanine) 是鸟嘌呤核苷酸结合蛋白G(I)/G(S)/G(O) γ -2亚基、髓鞘碱性蛋白、GTP-结合核蛋白 Ran、原肌球蛋白 α - 4链、HIV-1 Rev 结合蛋白2、Xaa-Pro 二肽酶、胸腺酶 β -10、肌动蛋白样蛋白3、丙氨酸转氨酶、丝氨酸/苏氨酸蛋白磷酸酶PP1 - β催化亚基、10 kda 热休克蛋白(线粒体)、钙调蛋白和 β -1-syntrophin 的底物。
T16381	Okadaic acid	Others	Others
	Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A, and PP3 inhibitor (IC50s: 10-15 nM, 0.5 nM, and 4 nM, respectively). Okadaic acid is extracted from black sponges of the genus Halic
T37055	Cytostatin
	Cytostatin is a natural antitumor inhibitor of cell adhesion to extracellular matrix, blocking adhesion of B16 melanoma cells to laminin and collagen type IV in vitro (IC50s = 1.3 and 1.4 μg/ml, respectively) and B16 cells metastatic activity in mice. It induces apoptosis of FS3 mouse fibrosarcoma cells (IC50 = 3.1 μg/ml). Cytostatin potently and selectively inhibits protein phosphatase 2A (PP2A; IC50 = 29 nM against the catalytic subunit), while having no effect against PP1, PP2B, or PP5.

天然产物

Cat.No: T4839

Synonym: N-Acetylalanine,N-Acetyl-L-alanine,N-乙酰-L-丙氨酸

Target: Others, Endogenous Metabolite

Cat.No: T16381

Target: Others

Cat.No: T37055

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